1H-Benzimidazole, 1-ribofuranosyl- | 14505-70-5

• 分子结构分类: 有机化合物 - 核苷、核苷酸和类似物 - 苯并咪唑核糖核苷和核糖核苷酸
• 英文名称: 1H-Benzimidazole, 1-ribofuranosyl-
• 英文别名: (3R,4S,5R)-2-(benzimidazol-1-yl)-5-(hydroxymethyl)oxolane-3,4-diol
• CAS: 14505-70-5
• 化学式: C₁₂H₁₄N₂O₄
• 分子量: 250.25
• InChiKey: VQJDOEMQZNKEMJ-KBIHSYGRSA-N

物化性质

• 沸点：
  554.5±60.0 °C(Predicted)
• 密度：
  1.62±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  -0.2
• 重原子数：
  18
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.42
• 拓扑面积：
  87.7
• 氢给体数：
  3
• 氢受体数：
  5

文献信息

• [EN] STEREOCHEMICALLY ENRICHED COMPOSITIONS FOR DELIVERY OF NUCLEIC ACIDS<br/>[FR] COMPOSITIONS ENRICHIES STÉRÉOCHIMIQUEMENT POUR L'ADMINISTRATION D'ACIDES NUCLÉIQUES
  申请人：SHIRE HUMAN GENETIC THERAPIES

  公开号：WO2015200465A1

  公开（公告）日：2015-12-30

  Provided, in part, is a composition comprising one or more chemical entities of formula I, each of which is a compound of formula (I):a pharmaceutically acceptable salt thereof, a solvate thereof, or a solvate of a pharmaceutically acceptable salt thereof, the composition characterized in that greater than a first threshold amount of the total amount of chemical entities of formula I in the composition: are chemical entities of formula I.a, wherein the first threshold amount is 50%; or are chemical entities of formula I.b.1, wherein the first threshold amount is 25%; or are chemical entities of formula I.b.2, wherein the first threshold amount is 25%, wherein the chemical entities of formula I.a, I.b.1, and I.b.2, are described herein, and methods of using such compositions, for example, for the delivery of a polynucleotide in vivo.

  提供的部分内容是一种组合物，包括一个或多个化学实体的公式I，其中每个化合物都是公式（I）的化合物：其药学上可接受的盐，其溶剂化物，或其药学上可接受的盐的溶剂化物，该组合物的特征在于公式I的化学实体的总量大于第一个阈值：其中第一个阈值为50％，公式I.a的化学实体的化学实体，或者是化学实体I.b.1，其中第一个阈值为25％，或者是化学实体I.b.2，其中第一个阈值为25％，其中公式I.a，I.b.1和I.b.2的化学实体在此处描述，以及使用这种组合物的方法，例如，在体内传递多核苷酸。
• Novel pharmaceutical agents containing carbohydrate moieties and methods of their preparation and use
  申请人：Christian T. Samuel

  公开号：US20060189547A1

  公开（公告）日：2006-08-24

  Hydrophilic N-linked pharmaceutical compositions, methods of their preparation and use in neuraxial drug delivery comprising a glycosyl CNS acting prodrug compound covalently N-linked with a saccharide through an amide or an amine bond and a formulary consisting of an additive, a stabilizer, a carrier, a binder, a buffer, an excipient, an emollient, a disintegrant, a lubricating agent, an antimicrobial agent or a preservative, with the proviso that the saccharide moiety is not a cyclodextrin or a glucuronide.

  亲水性N-连接药物组合物，其制备方法和在神经轴向药物输送中的使用，包括一种糖基中枢神经系统作用前药化合物，通过酰胺或胺键与糖苷共价连接，并且配方包括添加剂、稳定剂、载体、粘合剂、缓冲剂、赋形剂、润肤剂、破碎剂、润滑剂、抗微生物剂或防腐剂，但前提是糖苷基团不是环糊精或葡萄糖醛酸盐。
• Transdermal delivery of pharmaceutical agents
  申请人：Russell-Jones J. Gregory

  公开号：US20070243132A1

  公开（公告）日：2007-10-18

  The present invention generally relates to a vehicle useful for delivering a pharmaceutically active compound including a genetic molecule or composition. More particularly, the present invention provides microemulsions for transdermal delivery of pharmaceutically active agents to a subject.

  本发明通常涉及一种用于传递包括遗传分子或组成的药物活性化合物的车辆。更具体地，本发明提供了微乳液，用于经皮途径向受体传递药物活性剂。
• Novel Pharmaceutical Agents Containing Carbohydrate Moieties And Methods Of Their Preparation And Use
  申请人：Christian Samuel T.

  公开号：US20110237544A1

  公开（公告）日：2011-09-29

  Hydrophilic N-linked pharmaceutical compositions, methods of their preparation and use in neuraxial drug delivery comprising a glycosyl CNS acting prodrug compound covalently N-linked with a saccharide through an amide or an amine bond and a formulary consisting of an additive, a stabilizer, a carrier, a binder, a buffer, an excipient, an emollient, a disintegrant, a lubricating agent, an antimicrobial agent or a preservative, with the proviso that the saccharide moiety is not a cyclodextrin or a glucuronide.

  亲水性N-连接的药物组成物、其制备方法和在神经轴药物输送中的使用，包括一种糖基CNS作用的前药化合物，通过酰胺或胺键与糖分子共价连接，并由添加剂、稳定剂、载体、粘合剂、缓冲剂、赋形剂、润肤剂、崩解剂、润滑剂、抗微生物剂或防腐剂组成的制剂，前提是糖分子部分不是环糊精或葡糖醛酸盐。
• Brain-specific drug delivery
  申请人：UNIVERSITY OF FLORIDA

  公开号：EP0262696A2

  公开（公告）日：1988-04-06

  The invention provides compounds adapted for the site-specific/sustained delivery of a centrally acting drug species to the brain having the formula [D-DHC] and the non-toxic pharmaceutically acceptable salts thereof, wherein [D] is a centrally acting drug species which is an anticancer/antitumor and/or antiviral agent, said drug species having a purine or pyrimidine base-type structure bearing a singly or multiply hydroxylated substituent, and [DHC] is the reduced, biooxidizable, blood-brain barrier penetrating, lipoidal form of a dihydropyridine ⇆ pyridinium salt redox carrier comprising at least one dihydropyridine ring system of the formula wherein R is lower alkyl or benzyl and the dotted line indicates the presence of a double bond in either the 2 or 3 position of the dihydropyridine ring, a ring carbon atom of each dihydropyridine ring system being connected via a bridging group to a reactive hydroxyl functional group in the centrally acting drug species. The corresponding quaternary derivatives are also described.

  本发明提供了适用于向大脑定点/持续递送中枢作用药物的化合物，其分子式为[D-DHC]及其无毒的药学上可接受的盐，其中[D]为中枢作用药物，是一种抗癌/抗肿瘤和/或抗病毒药物、DHC]是二氢吡啶⇆吡啶鎓盐氧化还原载体的还原型、可生物氧化的、可穿透血脑屏障的脂质形式，该载体包含至少一个二氢吡啶环系统，其式为 其中 R 为低级烷基或苄基，虚线表示在二氢吡啶环的 2 位或 3 位存在双键，每个二氢吡啶环系统的环碳原子通过桥基与中心作用药物种类中的活性羟基官能团相连。还描述了相应的季衍生物。